| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H24ClN3O |
| Molecular Weight | 381.898 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCC[C@@H](CC1)N2N=C(CC3=CC=C(Cl)C=C3)C4=C(C=CC=C4)C2=O
InChI
InChIKey=MBUVEWMHONZEQD-SFHVURJKSA-N
InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3/t18-/m0/s1
Azelastine (brand names AZEP, ASTEPRO, ASTELIN etc.) a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is a potent antiallergic compound with histamine H1-receptor antagonist activity and a rapid onset and long duration of action. The major metabolite, desmethylazelastine, also exhibits H1-
receptor antagonist activity. AZEP Nasal Spray is administered as a racemic mixture.
The racemate, R- and S- enantiomers were equally potent at inhibiting eyelid
histamine-induced oedema in rats, however the R-enantiomer was 2-fold less active
at inhibiting eyeball histamine-induced oedema.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Adults and children aged 5 years and over:Each spray contains 125 ug of azelastine (as hydrochloride).One spray into each nostril twice daily as necessary (equivalent to a daily dose of 0.50 mg azelastine
Route of Administration:
Nasal
SUBSTANCE RECORD
